Pyrrolidinylalkylcarboxylic acid amide derivatives, their preparation and pharmaceutical compositions containing them

Abstract

2-Oxo-1-pyrrolidinylalkylcarboxylic acid amides of formula I ##STR1## in which R represents a hydrogen atom or hydroxy group, R 1 represents a hydrogen atom or a methyl group and R 2 represents a substituted or unsubstituted pyridyl group or a substituted phenyl group, the substitution being by from 1 to 3 substituents, which may be the same or different selected from halogen atoms, trifluoromethyl, nitro and acetyl groups, straight or branched-chain alkyl groups having 1-4 carbon atoms, alkoxy groups having 1-4 carbon atoms, straight or branched-chain alkylmercapto groups having 1-7 carbon atoms, substituted alkylmercapto groups of the general formula II ##STR2## in which n represents 1 or 2, R 3 is a hydrogen atom or a methyl group and R 4 is a hydroxy group or an amino group of the general formula V ##STR3## in which R 8 represents a hydrogen atom or methyl group and R 9 represents a methyl group or substituted or unsubstituted benzyl group, or R 8 and R 9 together with the nitrogen atom shown in formula V, form a substituted pyrrolidine ring; sulphonyl groups of the general formula III --SO.sub.2 R.sub.5 III in which R 5 represents an --NH 2 group or an alkyl group having 1-3 carbon atoms; and aminoethoxycarbonyl groups of the general formula IV ##STR4## in which each of R 6 and R 7 , which may be the same or different, represents a hydrogen atom or methyl or ethyl group; and the pharmaceutically tolerable acid addition salts of compounds of formula I having a basic nitrogen atom are useful in treating cerebral circulatory disturbances, cerebro-atrophic crises and cerebral ageing processes.

We claim: 
     
       1. 2-oxo-1-pyrrolidinylalkylcarboxylic acid amides of the general formula I ##STR92## in which R is selected from the group consisting of hydrogen and hydroxyl and R 1  is selected from the group consisting of hydrogen and methyl, and the pharmaceutically tolerable acid addition salts of compounds of formula I having a basic nitrogen atom. 
     
     
       2. Compounds according to claim 1 wherein R is hydrogen. 
     
     
       3. As a compound according to claim 1, 2-oxo-1-pyrrolidinylacetic acid 2,6-dimethylanilide. 
     
     
       4. As a compound according to claim 1, 4-hydroxy-2-oxo-1-pyrrolidinylacetic acid 2,6-dimethylanilide. 
     
     
       5. A pharmaceutical composition for the treatment of cerebral circulatory disturbances, comprising in a therapeutically effective amount at least one compound defined in any one of claims 1, 3, or 4 and a pharmaceutically acceptable excipient. 
     
     
       6. A method of treating a patient for cerebral circulatory disturbance, which comprises administering to the patient a therapeutically effective dose of at least one compound defined in any one of claims 1, 4 or 5.